CURCUMIN MICROENCAPSULATION USING CHITOSAN–ETHYL CELLULOSE–GMS MIXTURE FOR PRESERVATION OF MUCOADHESIVE PROPERTIES AND CONTROLLED RELEASE KINETIC

Objective: This research aimed to prepare curcumin microcapsules by the spray drying method and to evaluate their characteristics. Methods: The microcapsules were prepared by the spray drying method. The generated microcapsules were evaluated for organoleptic, morphology, particle size, the percentage of curcumin and water content. Furthermore, the release of curcumin from the microcapsules was tested in vitro and compared to uncoated curcumin powder. In addition, the mucoadhesive properties of uncoated curcumin powder and curcumin microcapsules were also evaluated. Results: The results showed that the microcapsules had spherical shape with particle size in the range of 100–1009 µm and water content of 9.34% (w/w) (FIII) and 8.09% (w/w) (FVI). The release of curcumin from its uncoated powder and the microcapsules FVI within 8 h were 8.87% and 26.32% (w/w), respectively. It was found that the mucoadhesive properties of microcapsules FVI were better than those of FIII and uncoated curcumin powder. Microcapsules FVI rendered the cumulative amount of curcumin remaining on the intestinal mucosa of 55% (w/w) within 3 h. Conclusion: Accordingly, curcumin microcapsules generated by spray drying could be further formulated into various solid dosage forms for a better therapeutic effect.

Recent Advances in the Excipients Used in Modified Release Vaginal Formulations

The formulation of an ideal vaginal drug delivery system (DDS), with the requisite properties, with respect to safety, efficacy, patient compliance, aesthetics, harmonization with the regulatory requirements, and cost, requires a meticulous selection of the active ingredients and the excipients used. Novel excipients defined by diversity and multifunctionality are used in order to ameliorate drug delivery attributes. Synthetic and natural polymers are broadly used in pharmaceutical vaginal formulations (solid, semi-solid dosage forms, implantable devices, and nanomedicines) with a promising perspective in improving stability and compatibility issues when administered topically or systemically. Moreover, the use of biopolymers is aiming towards formulating novel bioactive, biocompatible, and biodegradable DDSs with a controllable drug release rate. Overviewing vaginal microenvironment, which is described by variable and perplexed features, a perceptive choice of excipients is essential. This review summarizes the recent advances on the excipients used in modified vaginal drug delivery formulations, in an attempt to aid the formulation scientist in selecting the optimal excipients for the preparation of vaginal products.

PHARMACEUTICAL MARKET ASSORTMENT RESEARCH OF DRUGS FOR VAGINAL USE WITH PROBIOTIC MEDICINES DETAILING

vaginal route delivery of drugs is an integral part of gynaecological diseases treatment including different genesis vulvovaginitis. The aim of this study it to analyze Ukrainian pharmaceutical market assortment of drugs for vaginal use with probiotic medicines determination. The marketing research was conducted with using of analysis, synthesis, comparison, generalization, content-analysis, statistical, graphical methods. The data of State register of medicines (as of June, 30, 2021), register of wholesale dispensing prices for medicines (as of June, 30, 2021), official web-sites LLC «Morion», «Pharmacy.online», «Compendium.online» were used as objects of the study. As a result, it is determined that as of June 30, 2021 142 medicines for vaginal use are registered on Ukrainian pharmaceutical market with dosage forms, active substances doses, condition for dispensing consideration, 100 brand names, 26 international nonproprietary names, 7 synonymous names. Structural ATC-classification analysis has shown that medicines for vaginal use are included in ATC-groups G «Genito urinary system and sex hormones» and D «Dermatologicals» The assortment macrocontour is formed, it demonstrates that 67,2% of drugs for vaginal use are involved in group G01A «Аntiinfectives and antiseptics, excluding combinations with corticosteroids». More than 80% of drugs for vaginal use are registered as solid dosage forms, and almost half of them as suppositories or pessaries. Almost 65% of medicines are foreign, and 3/4 of them contain only active substance, more than 50% are prescription only medicines. For 44,4% drugs for vaginal use the storage period of 3 years (36 months) is determined. Detailing analysis of medicines with probiotic activity has shown assortment deficiency (only 3 brand names are registered). The liquidity coefficients calculations for this brand manes don’t allow to characterize these drugs as economically affordable. The obtained results of this study inform about the domestic drugs for vaginal use with probiotic activity development relevance, especially in pessaries as dominant dosage form on the pharmaceutical market.

Solid Dosage Forms of Biopharmaceuticals in Drug Delivery Systems Using Sustainable Strategies

Drug delivery systems (DDS) often comprise biopharmaceuticals in aqueous form, making them susceptible to physical and chemical degradation, and therefore requiring low temperature storage in cold supply and distribution chains. Freeze-drying, spray-drying, and spray-freeze-drying are some of the techniques used to convert biopharmaceuticals-loaded DDS from aqueous to solid dosage forms. However, the risk exists that shear and heat stress during processing may provoke DDS damage and efficacy loss. Supercritical fluids (SCF), specifically, supercritical carbon dioxide (scCO2), is a sustainable alternative to common techniques. Due to its moderately critical and tunable properties and thermodynamic behavior, scCO2 has aroused scientific and industrial interest. Therefore, this article reviews scCO2-based techniques used over the year in the production of solid biopharmaceutical dosage forms. Looking particularly at the use of scCO2 in each of its potential roles—as a solvent, co-solvent, anti-solvent, or co-solute. It ends with a comparison between the compound’s stability using supercritical CO2-assisted atomization/spray-drying and conventional drying.